A non-crosslinking platinum-acridine hybrid agent shows enhanced cytotoxicity compared to clinical BCNU and cisplatin in glioblastoma cells

Bioorg Med Chem Lett. 2005 Jan 17;15(2):443-6. doi: 10.1016/j.bmcl.2004.10.049.

Abstract

Using clonogenic survival assays, we demonstrated that a new platinum-acridine hybrid agent, PT-ACRAMTU, is cytotoxic in SNB19 and U87MG glioblastoma cells at low-micromolar concentrations. PT-ACRAMTU is more cytotoxic than ACRAMTU (the platinum-free acridine), acts in a time and dose dependent manner, and appears to generate an apoptotic response in both cell lines on the basis of increased caspase-3 activity.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Acridines / chemistry*
  • Acridines / pharmacology
  • Acridines / toxicity
  • Animals
  • Carmustine / pharmacology*
  • Carmustine / toxicity
  • Caspase 3
  • Caspases / metabolism
  • Cell Line
  • Cisplatin / pharmacology*
  • Cisplatin / toxicity
  • Cross-Linking Reagents / pharmacology
  • Cross-Linking Reagents / toxicity
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Glioblastoma / pathology
  • Inhibitory Concentration 50
  • Organoplatinum Compounds / pharmacology
  • Organoplatinum Compounds / toxicity
  • Platinum / chemistry*
  • Platinum / pharmacology
  • Platinum / toxicity

Substances

  • Acridines
  • Cross-Linking Reagents
  • Organoplatinum Compounds
  • Platinum
  • Caspase 3
  • Caspases
  • Cisplatin
  • Carmustine